Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Product Details of 7025-19-6. Introducing a new discovery about 7025-19-6, Name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid
Structure-guided design of thiazolidine derivatives as mycobacterium tuberculosis pantothenate synthetase inhibitors
The pantothenate biosynthetic pathway is essential for the persistent growth and virulence of Mycobacterium tuberculosis (Mtb) and one of the enzymes in the pathway, pantothenate synthetase (PS, EC: 6.3.2.1), encoded by the panC gene, has become an appropriate target for new therapeutics to treat tuberculosis. Herein, we report nanomolar thiazolidine inhibitors of Mtb PS developed by a rational inhibitor design approach. The thiazolidine compounds were discovered by using energy-based pharmacophore modelling and subsequent in vitro screening, which resulted in compounds with a half maximal inhibitory concentration (IC50) value of (1.12¡À0.12) muM. These compounds were subsequently optimised by a combination of modelling and synthetic chemistry. Hit expansion of the lead by chemical synthesis led to an improved inhibitor with an IC50 value of 350 nM and an Mtb minimum inhibitory concentration (MIC) of 1.55 muM. Some of these compounds also showed good activity against dormant Mtb cells. Let sleeping cells lie: Mycobacterium tuberculosis pantothenate synthetase (Mtb PS) has become a target for new therapeutics to treat tuberculosis. Nanomolar thiazolidine inhibitors of Mtb PS were developed by rational inhibitor design involving modelling, in vitro screening and optimisation. Hit expansion of the lead by synthesis led to an improved inhibitor with an IC50 value of 350 nM and an Mtb MIC value of 1.55 muM. Some of these compounds also showed good activity against dormant Mtb cells.
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Product Details of 7025-19-6, you can also check out more blogs about7025-19-6
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